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United States Patent |
5,059,603
|
Rubin
|
October 22, 1991
|
Method and composition for treating impotence
Abstract
A composition for treating impotence contains a vasodilator, a
vasoconstrictor, and a penetration enhancing ingredient in a
pharmaceutically acceptable carrier for topical application. The
composition is applied topically to treat impotence.
Inventors:
|
Rubin; David (San Diego, CA)
|
Assignee:
|
Centuries Laboratories, Inc. (Port Washington, NY)
|
Appl. No.:
|
364289 |
Filed:
|
June 12, 1989 |
Current U.S. Class: |
514/263.31; 514/742; 514/947 |
Intern'l Class: |
A61K 031/52 |
Field of Search: |
514/264,367,415,947,647,742,248
424/608
|
References Cited
U.S. Patent Documents
2550398 | Apr., 1951 | Barol.
| |
3483870 | Dec., 1969 | Coover, Jr. et al.
| |
3740420 | Jun., 1973 | Herschler et al.
| |
3896238 | Jul., 1975 | Smith | 424/358.
|
3953599 | May., 1976 | MacMillan et al. | 424/265.
|
4127118 | Nov., 1978 | Latorre | 128/79.
|
4285967 | Aug., 1981 | Gubernick et al. | 424/289.
|
4444762 | Apr., 1984 | Rajadhyaksha | 424/180.
|
4557934 | Dec., 1985 | Cooper | 514/399.
|
4575515 | Mar., 1986 | Sandborn | 514/708.
|
4743588 | May., 1988 | Mirejovsky et al. | 514/24.
|
4746675 | May., 1988 | Makino et al. | 514/423.
|
4764379 | Aug., 1988 | Sanders et al. | 424/449.
|
4764381 | Aug., 1988 | Bodor et al. | 424/449.
|
4789667 | Dec., 1988 | Makino et al. | 514/161.
|
4795756 | Jan., 1989 | Oxford et al. | 514/415.
|
4801586 | Jan., 1989 | Minaskanian et al. | 514/212.
|
4801587 | Jan., 1989 | Voss et al. | 514/248.
|
4808414 | Feb., 1989 | Peck et al. | 424/449.
|
Other References
Morales et al., Urologic Clinics of North America 15: (1) 87-93, 1988.
Moshikov, Chemical Abstracts vol. 52, 1958, Abstract 5637h.
Ilarionov et al., Chem. TBS. vol. 111, No. 11 entry #89683f (1989).
Barbanti et al., Urol. Res. vol. 16 (4) pp. 299-302. (1988).
Kiely et al., British J. Vrol. vol. 59 (4) pp. 334-339 (1987).
|
Primary Examiner: Shah; Mukund J.
Assistant Examiner: Ward; E. C.
Attorney, Agent or Firm: Browdy and Neimark
Claims
What is claimed is:
1. A composition for treating impotence consisting essentially of an
effective amount of nitroglycerine as a vasocilator and an effective
amount of caffeine as a vasoconstrictor, and a penetration enhancer, in a
pharmaceutically acceptable carrier.
2. The composition according to claim 1 wherien said penetration enhancer
is dimethylsulfoxide.
Description
FIELD OF THE INVENTION
The present invention relates to a composition and method for treating
impotence.
BACKGROUND OF THE INVENTION
Impotence, or lack of a man's ability to have sexual intercourse, is often
the subject of parlor humor, but millions of men suffer from this
condition, regardless of age, Impotence is generally characterized by an
inability to maintain a penile erection.
Causes of impotence are numerous. It may be atonic, due to paralysis of the
motor nerves (nervi erigentes) without any evidence of lesions to the
central nervous system. Conversely, it could be paretic as a results of a
lesion in the central nervous system, particularly the spinal cord.
Alternatively, it could be psychic, and dependent on a mental problem or
instability. Finally, it could be symptomatic, due to some other disorder,
such as injury to nerves in the perineal region, by virtue of which the
sensory portion of the erection reflex is blocked out.
Whether the impotence is absolute, involving all sexual modalities, total,
affecting all sexual function, though not necessarily libido, or partial,
affecting the rigidity or duration of the erection, or whether the cause
of impotence is organic, due to structural changes, disease, or some
demonstrable functional impairment anywhere in the sexual system,
psychogenic, due to old age or sexual satiation, the result is the same:
at least partial inability to engage in sexual activity due to the lack of
an adequate erection.
Impotence may be defined more fully, however, as the inability to develop
or sustain an erection of the penis sufficient to conclude coitus or
orgasm and ejaculation to the male's own satisfaction. Impotence treatment
methods are generally, however, concerned with the erection aspect, and
not ejaculatory impotence, which is relatively rare.
The body of the penis is surrounded by a cornified layer of skin. Blood is
supplied through the dorsal artery and removed through the dorsal vein.
The urethra is surrounded by a fibrous compartment known as the corpus
songiosum, which permits urination and provides a path for semen during
ejaculation.
The corpora cavernosa form the chief part of the body of the penis, and at
their rear portion they form the crura where the penis is firmly connected
to the pelvis and ischium. The corpora cavernosa are surrounded by a
fibrous sheath having exterior and interior portions respectively. The
portion of the corpora cavernosa within the fibrous sheath consists of a
sponge-like tissue of arveolar spaces freely communicating with each other
and filled with venous blood. This space may be thought of as a large
cavernous vein. The arteries bringing blood to these spaces are the
arteries of corpora cavernosa and branches from the dorsal artery, which
perforate the fibrous sheath along the upper surface thereof.
Under the proper stimulus, the penis becomes erect when the corpora
cavernosa become widely dilated with arterial blood, thereby causing these
tissues to become less flaccid. At the extreme side of the corpus
cavernosum, tiny veins are connected to nerve endings, and, upon the
proper stimulus, the veins assume a position so as to block outflow of
blood from the corpus cavernosum. This mechanism is psychologically
controlled.
The turgor phenomenon is generally caused by an action of the autonomic
nervous system. The autonomic nervous system consists of two divisions,
the sympathetic nervous system and the parasympathetic nervous system. In
a healthy individual, activity by one of the two autonomic nervous system
results in a physiological effect opposite to that of the activity of the
other system. An autonomically-controlled physiological state is
determined, at any time, by the relative degree of activity of the two
systems.
The autonomic system controls the blood flow in the penis by means of
peripheral nerves attached to the arterial vessels in and around the
corpora cavernosa. During normal physiological activity, the sympathetic
nerves maintain these arteries in a constricted state. As the man becomes
aroused, his parasympathetic system releases certain chemicals,
principally catecholamines such as norepinephrine and epinephrine, which
inhibit the action of the sympathetic nerves resulting in relaxation of
the smooth muscles surrounding the arteries and thus dilation thereof.
In the case of neurological problems, the nerves cannot convey the proper
stimulus to either the arteries or the veins, This is the case with
diabetics or patients with problems of the peripheral nervous system. In
the case of a patient afflicted with arteriosclerosis, which often
accompanies aging, the arteries cannot carry sufficient blood to the
corpus cavernosum because of obstruction.
The most widely used therapy for treating impotence has been the
implantation of penile prostheses. The simplification of the surgical
technique, the obvious and rapid solution of the difficulties for
intromission, and the popular appeal of prostheses all inhibited the
search for pharmacologic intervention. However, recently, a great interest
has developed in the use of a variety of agents for improving both libido
and the quality of erections.
Many blood constrictive devices have also been proposed for producing and
enhancing an erection. Typically, these are adjustable, tourniquet-like
rubber band devices which are designed to fit tightly around the shaft of
the penis and thereby restrict the flow the blood from the penis through
the surface veins, as well as the deeper dorsal vein, to prolong an
erection. There have been numerous attempts to solve this problem, but all
exhibit various disadvantages to the user, and sometimes to the female
partner, such as extreme discomfort during intercourse, to the extent that
users might not achieve the desired usefulness as frequently as desired
and to the extent preferred. All of the external devices previously
proposed have the psychological disadvantages of being an impediment to
actual intercourse, and the operational disadvantage that their duration
of effectiveness is relatively short.
Impotence associated with androgen deficiency has long been thought by
certain medical factions to be treatable by the administration of male
hormones via synthetic preparations such as methyl testosterone and
various esters, as well as a number of testosteroneaphrodisiac
compositions. The relationship between testosterone levels and impotence
has not been firmly established. However, the administration of exogenous
hormones has several pharmacologic disadvantages. For example, methyl
testosterone must be taken subcutaneously or bucally, and may cause severe
toxic effects such as cholestatic jaundice. Parenterally administered
testosterone esters, while less toxic and more certainly absorbed than
methyl testosterone, have the drawbacks of intramuscular administration
including additional pain, lack of complete absorption, and risk of deep
and widespread infection. Additionally, long-term administration of these
synthetic compounds may inhibit endogenous testosterone formation and
spermatogenesis by suppressing pituitary gonadotropin, resulting in
glandular tissue atrophy because of disuse.
Because of the uncertainty and the problems involved in the administration
of testosterone in the treatment of impotence, there have been numerous
nonandrogen attempts to treat the impotence problem, including treatments
with yohimbine, damiana, ginseng, levodopa, hydergine, clomiphene,
phosphorous, strychnine, and cantharides. Other drugs tested for treating
impotence include bromocriptine, nitroglycerin, zinc, oxytocin, and
lutenizing hormone-releasing hormone. These are generally administered
orally with varying degrees of success, some with significant side
effects.
Intracorporeal injections of papaverine have been investigated for some
time, and this has become one of the more commonly used of the various
pharmacologic agents. Alternatively, as disclosed by Latorre in U.S. Pat.
No. 4,127,118, nonsteroidal agents, including an appropriate vasodilator,
can be injected into the corpus cavernosa to cause an erection. Among the
vasodilators that can be used are sympathomimetic amines or adrenergic
blocking agents, or other agents within the histamine and epinephrine
groups. The most obvious drawback to this type of treatment is the need
for an infection whenever an erection is desirable.
Topical agents have also been proposed to induce an erection, such as
disclosed in Voss et al., U.S. Pat. No. 4,801,587. The ointment disclosed
therein comprises a vasodilator or alpha-blocker in an ointment base,
along with a carrier. However, in this case, the ointment only includes an
agent to dilate the arterial vessels, and there is nothing to constrict
the veins to retain the blood in the corpora cavernosa.
Nitroglycerin paste has been widely used in the treatment of angina.
Morales et al., in Urologic Clinics of North America 15:(1) 87-93, 1988,
disclose the results of a double-blind, controlled randomized trial of
nitroglycerin paste versus placebo paste under strictly controlled
laboratory conditions. This study demonstrated that nitroglycerin
transcutaneously administered enhances the quality of erectile episodes in
the presence of an erotic stimulus and under laboratory conditions. An
important consideration is the effect of the drug on the sexual partner,
since nitroglycerin is readily absorbed by the vaginal mucosa. One case of
secondary headache in the sexual partner of an individual who used
nitroglycerin on his penis has been reported.
SUMMARY OF THE INVENTION
It is an object of the present invention to overcome the above-noted
deficiencies in the prior art.
It is another object of the present invention to provide a composition for
treating impotence.
It is a further object of the present invention to provide a method for
treating impotence.
It is still another object of the present invention to provide an improved
method of treating impotence without afflicting the partner with secondary
headaches.
According to the present invention, impotence is treated by transcutaneous
administration of a combination of a vasodilator and a vasoconstrictor in
a carrier including an agent to assist absorption of the active
ingredients through the skin around the penis. The vasodilator and
vasoconstrictor are chosen so that the vasodilator acts more quickly than
the vasoconstrictor. When the vasodilator enters the corpora cavernosa
within the penis, it causes dilation of the corpora, resulting in an
erection. Then, when the later-acting vasoconstrictor enters the corpora
cavernosa, it causes the veins to constrict and thus retain the blood in
the erect penis to enhance the erection. A topically applied
antiinflammatory agent can be used to prevent local irritation of the
skin.
The composition of the present invention is topically applied, and thus can
be incorporated in any suitable carrier. The active ingredients can be
present in the composition in amounts ranging from approximately 0.05 to
5.0% by weight of vasodilator, from about 0.05 to about 5.0% by weight of
vasoconstrictor, and from about 50 to about 90% of penetration-enhancing
agent. Any carrier suitable for topical administration can be used. Where
an antiinflammatory agent is used, it can be present in amounts ranging
from about 0.05 to about 1% by weight.
DETAILED DESCRIPTION OF THE INVENTION
Impotence can be treated by topical application of a composition containing
a vasodilator, a later-acting vasoconstrictor, and an absorption enhancing
agent in a pharmaceutically acceptable carrier. The vasodilator provides
almost immediate blood vessel congestion. The vasoconstrictor is absorbed
less quickly, perhaps three to four minutes later, and serves to retain
the blood in place. An anti-inflammatory agent can be used to prevent or
minimize local irritation of the skin.
While any vasodilator that adequately opens the blood vessels will suffice
for the treatment of impotence according to the present invention, the
preferred drugs are those which produce vasodilation by direct action on
the arteries themselves. This includes vasodilators or alpha-blockers
which can be administered topically, including nitroglycerin, papaverine
(6,7-dimethoxyl-1-veratrylisoquinoline), hydralzaine, sodium
nitroprusside, phenoxybenzamine, isoxaprine hydrochloride, nylidrin
hydrochloride, tolazoline hydrochloride, nicotinyl alcohol, and
phentolamine. A single application should contain between one and 5
milligrams of the vasodilator.
Of these drugs, nitroglycerin is currently extensively used in treatment of
angina pectoris, and is a well known vasodilator. Nylidrin is a
sympatomimetric amine, and exerts a pharmacologic action on skeletal
muscle blood vessels similar to that of epinephrine. Nylidrin increases
blood flow by a direct vasodilating action on the arteries, and has no
significant effect on pulse rate or blood pressure.
Isoxsuprine hydrochloride increases blood flow by direct relaxation of the
vascular musculature. This drug also has a slight adrenergic blocking
action, but this is not essential to its vasodilating effect. This drug is
conventionally used in treating certain obliterative vascular diseases
such as arteriosclerosis and andarteritis obliterans, and in vasospastic
diseases.
Tolazoline is an adrenergic blocking agent related structurally to both
histamine (a vasodilator) and epinephrine. Tolazoline also acts by a
direct dilating effect on the walls of blood vessels, and provides a
sympathetic block, probably at the terminations of sympathetic nerves. It
also has an anti-adrenergic effect which blocks the vasoconstrictive
action of epinephrine and levarterenol. While tolazoline traditionally is
administered orally in the treatment of various peripheral vascular
disorders, the preferred dosage for use topically in the present invention
is from about 10 to about 25 milligrams.
Nicotinyl alcohol is converted to nicotinic acid in the body to produce
peripheral vasodilation, thereby increasing blood flow to extremities when
administered orally. The preferred topical dosage for use in treating
impotence according to the present invention ranges from about 10 to about
25 milligrams. A disadvantage of this drug is that side effects such as
flushing of the face and gastrointestinal disturbances may result,
particularly at high dosage. However, side effects should generally be
minimal with the dosage of the present invention.
The vasoconstrictors which can be used in the present invention include
those vasoconstrictors which can be administered topically, including
caffeine, a well known ingredient in coffee and tea. A variety of other
vasoconstrictors can be used in the present invention, including
3-(2-aminoethyl)indole derivatives, described more fully in U.S. Pat. No.
4,795,756, to Oxford et al., and hereby incorporated by reference. These
compounds have traditionally been used for treatment of migraine
headaches, and in the method of the present invention are administered in
dosages of from about 0.1 to 00 mg. Another group of vasoconstrictors that
can be used in the present invention is the adrenergic agents including
pressor amines of the .beta.-phenylethylamine type, including epinephrine,
also known as adrenaline. Examples of other compounds of this type are
given in U.S. Pat. No. 3,483,870, to Coover, Jr. et al., which patent is
hereby incorporated by reference. These compounds are generally used in
amounts ranging from about 1 to about 200 mg per dose in the present
invention, and are generally chosen so that they act somewhat later than
the vasodilators with which they are combined in the compositions
according to the present invention.
The absorption or penetration enhancers most preferably used in the
compositions according to the present invention are the aliphatic
sulfoxides of the formula RSOR', wherein R is an alkyl, substituted alkyl,
alkenyl, or hetero group containing up to 12 carbon atoms, and R' is a low
molecular weight alkyl or hydroxy-substituted alkyl group. The most
commonly used of these, and the compound preferably used in the present
invention, is dimethylsulfoxide. The compositions according to the present
invention must contain at least about 50% dimethylsulfoxide in order to
achieve efficient, cient, practical penetration of the skin barrier. Lower
concentrations may thus result in less than the desired effect. On the
other hand, with very high concentrations of dimethylsulfoxide, such as
substantially above about 95%, the undesired side effects of local skin
irritation and dehydration, erythema, and urticaria increase markedly,
while no substantial increased benefit is obtained, and the rate of
penetration of the active ingredients may actually be lessened. In the
present invention, for dermal application, diluting the dimethylsulfoxide
with an appropriate diluent can minimize these side effects and enhance
acceptability of the compositions. Therefore, for a highly advantageous
administration of dimethyl sulfoxide to the intact skin, because of the
unusual penetration properties of the dimethylsulfoxide, compositions
containing from about 50% to about 90% dimethylsulfoxide with a
pharmaceutically acceptable diluent have been found to be uniquely
suitable and desirable. Dimethylsulfoxide-glycerin solutions of 10% to 40%
glycerin content are quite advantageous to minimize skin irritation both
from the dilution of the dimethyl sulfoxide and the emollient. effects of
the glycerin, which tends to sooth the irritation and skin dryness which
may be caused by the dimethyl sulfoxide.
A number of other penetration enhancers can be used in the compositions
according to the present invention. Among these are optically active or
inactive pyroglutamates of the following formula
##STR1##
wherein R is a linear, branched, or cyclic alkyl or alkenyl group having
from 10 to 14 carbon atoms. These pyroglutamic esters are contained in
large amounts in human skin, and are among the natural moisturizing
factors in skin.
Among other penetration enhancers that can be used in compositions
according to the present invention are glycerol monolaurate,
dimethylacetamide, propylene glycol, or other organic esters such as
diisopropyl adipate or isopropyl myristate. Additional penetration
enhancers for use in compositions according to the present invention
include surfactants such as sodium laurylsulfate and
polyoxyethylene-2-sorbitan monolaurate. U Another effective penetration
enhancer for use in the present invention is 2-ethyl-l,3-hexanediol either
alone or in combination with oleic acid.
Another group of compounds which are useful in the present invention are
penetration enhancers of the formula
##STR2##
wherein R.sub.1 and R.sub.2 are identical or different and each represents
H, a C.sub.1-25 alkyl, C.sub.2.congruent. alkenyl, a (C.sub.1-24 alkyl)
carbonyl or a (C.sub.2-24 alkenyl) carbonyl, provided that R.sub.1 and
R.sub.2 are not H at the same time, or R.sub.1 and R.sub.2, taken
together, may form a group of the following formula:
##STR3##
in which R.sub.3 and R.sub.4 are identical or different and each represents
H, C.sub.1-24 alkyl, or C.sub.1-24 alkenyl.
Another group of penetration enhancing agents includes amides of
heterocyclic amines of the following structural formula:
##STR4##
wherein m is from 4 to 9;
R.sub.1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and
R is a straight or branched chain alkyl group having from 1 to 20 carbon
atoms.
Yet another group of penetration enhancers that can be used in the present
invention are 1-substituted azacyclopentan-2-ones, as described in more
detail in U.S. Pat. No. 4,444,762 to Jajadhyaksha, which patent is hereby
incorporated by reference. These compounds have the structural formula:
##STR5##
wherein R' is H or a lower alkyl group; m is from 3 to 7;
n is from 0-17; and
R is --CH.sub.3, phenyl, substituted phenyl, or
##STR6##
with the proviso that if m is 3 and R is --CH.sub.3, then n is not from 0
to 6. These compounds can be used either alone or with C.sub.3 -C.sub.5
diols.
Amides of the formula
##STR7##
wherein R.sup.1 and R.sup.2 are independently selected from the group
consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to
20 carbon atoms and R is selected from the group consisting of alkyl
radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms, and
the total number of carbon atoms in the compound is at least 15. These
compounds are described more fully in U.S. Pat. No. 4,808,414, to Peck et
al., which patent is hereby incorporated by reference.
Sugar esters on combination with a sulfoxide or phosphine oxide can also be
used to enhance penetration of the active ingredients. These sugar esters
include hydrocarbyl and alkyl polyoxyalkylene esters of cyclic polyhydroxy
saccharides wherein at least one of the hydroxyl groups on the saccharide
moiety is substituted with an acyl or polyoxyalkylene group. These
compounds are described in more detail in U.S. Pat. No. 3,896,238, to
Smith, which patent is incorporated herein by reference.
The compositions of the present invention may be formulated into highly
convenient dosage forms with thickening agents, including thickened
solutions or lotions, ointments (including creams and gels), and the like.
Thickened solutions or lotions and ointments may be formed by incorporating
with the penetration enhancer and the active ingredients, various gelling
agents or other thickeners (viscosity increasers) which permit release of
the active ingredients to the skin upon application. These forms are
advantageously employed to lessen the runoff from the skin that may occur
with the more fluid composition forms. Importantly, they also permit more
sustained contact of the penetration enhancer with the treated surfaces,
thus enhancing the speed of delivery of the active ingredients
subcutaneously, and providing more accurate and controllable dosing.
Accidental spilling and undesired contact with the material can also be
minimized with these types of formulations.
It is advantageous to use water-dispersible thickening agents (i.e., agents
dispersible in water to form a homogeneous distribution or solution), such
as the polyethylene glycols, as they are readily compatible with water or
other diluents to be formulated in the compositions, and they may be
readily washed from the skin following absorption into the skin of the
active ingredients. Alternatively, an emulsion base may be used to impart
the desired thickening effect, together with the emollient effect of the
lipoid phase of the emulsion base, a better spreading and wetting effect
and a retardation of any skin-drying effect of the penetration enhancing
compounds. When compositions are formulated with an emulsion base, the
penetration enhancer is incorporated in the water phase thereof. Another
category of thickening base which can also impart an emollient effect is
provided by lipoidal thickening agents which are soluble in the
penetration enhancer.
The water-soluble thickening bases may use polyethylene glycols of
different viscosities, depending upon the desired consistency and
concentration of penetration enhancer and vasodilator and vasoconstrictor
to be incorporated in the compositions. Other thickening agents include
water-dispersible gums, carboxyvinyl polymers, methyl cellulose, sodium
carboxymethyl cellulose, alginates, and the like.
Lotions and ointments incorporating emulsion bases may contain the usual
ingredients to provide the base, including fatty alcohols such as acetyl
alcohol, an emulsifier such as lauryl sulfate, and water.
Pourable pharmaceutical dosages may be provided and dispensed in graduated
containers, or containers which contain a given volume, such as 5 cc or
the like. Containers with columns of 20 cc and above provide convenient
multiple dosage forms, and those containing a typical single dose, such as
from about 05.g to about 10 grams of a combination of vasodilator,
vasoconstrictor, and penetration enhancer, provide convenient dosage
forms. Squeeze tubes for lotions and ointments and cotton stick
applicators may all be used for topical application of the thickened
compositions.
The compositions of the present invention can also be administered by
spraying and misting such as from misting devices and aerosol bottles,
which containers are charged with fluid formulations containing at least
10% by weight of a combination of penetration enhancer, vasodilator, and
vasoconstrictor, along with an aqueous diluent and, optionally, thickening
agents, physiological salts, and the like. These compositions can be
administered as either liquids or semisolid gels or mousses, depending
upon the amount of gelling agents or surfactants included in the
compositions. Compositions for this purpose are sufficiently fluid to
permit dispensing by spray or mist from the container, and also meet the
previously described criteria for penetrability and avoidance of undue
side effects.
The following nonlimiting examples illustrate the compositions and dosage
forms of this invention, and techniques for their preparation:
EXAMPLE 1
A liquid formulation is made from 750 mg nitroglycerine, 750 mg caffeine,
500 mg hydrocortisone, and 50 ml of dimethylsulfoxide in 40 ml distilled
water. This composition may be applied topically in amounts of 0.1 to 5 g
per application, generally by use of a cotton-tipped applicator.
EXAMPLE 2
An ointment is formulated from the following ingredients:
______________________________________
nitroglycerin 500 mg
caffeine 250 mg
stearic acid 40 g
acetyl alcohol 5 g
triethanolamine 4.2 g
glyceryl monostearate 4.2 g
water 40 ml
dimethylsulfoxide 80 ml
______________________________________
EXAMPLE 3
A spray composition according to the present invention is formulated as
follows:
A 50% dimethylsulfoxide solution in isotonic saline is transferred to a 50
cc resilient plastic bottle, and 500 mg of nitroglycerine, 750 mg of
caffeine, and 500 mg of hydrocortisone are added to the solution. A
closure with a spray orifice is affixed to the bottle, from which the
composition can be sprayed for topical administration.
EXAMPLE 4
A propellant spray composition is compounded from 50 ml water, 50 ml
dimethyl sulfoxide, 1.5 nitroglycerin, glycerin, 1.5 g caffeine, 500 mg
hydrocortisone, and a sufficient amount of propellent to provide a
propellant force.
EXAMPLE 5
An ointment is prepared from the following ingredients:
______________________________________
papaverine 400 mg
epinephrine 400 mg
stearic acid 30 g
triethanolamine 4 g
glyceryl monostearate 4 g
water 80 ml
dimethylsulfoxide 80 ml
______________________________________
EXAMPLE 6
A lotion formulation is prepared from the following ingredients:
______________________________________
niocotinyl alcohol 500 mg
caffeine 500 mg
propylene glycol 80 ml
glycerin 20 ml
water 10 ml
______________________________________
EXAMPLE 7
A liquid preparation for treating impotence by topical application thereof
is formulated from the following ingredients:
______________________________________
isoxsuprine hydrochloride
300 mg
caffeine 300 mg
polyoxyethylene-2-sorbitan
60 ml
monolaurate
distilled water 50 ml
hydrocortisone 300 mg
______________________________________
To treat impotence, the composition of the present invention is topically
applied to the penis to cause an erection. Generally, amounts ranging from
about 0.1 gram to about 5 grams of the composition are sufficient to be
effective, although the determination of the effective amounts is well
within the skill of the art.
Use of the subject invention in alleviating the problems of impotence is
far superior to most other methods since it is substantially unobtrusive
and is something of which the female sex partner need not be aware. Since
this method of treatment provides vasodilation without treatment of the
nervous aspect of inducing an erection, and includes vasoconstriction to
retain the blood in the proper area, the erection may be sustained for a
substantial period of time. In contrast, treatment involving devices to
produce local stimulation, thereby inducing an erection, will sustain the
erection for only a short period of time, since the nervous fibers are
fatigued after a short time.
The foregoing description of the specific embodiments will so fully reveal
the general nature of the invention that others can, by applying current
knowledge, readily modify and/or adapt for various applications such
specific embodiments without departing from the generic concept, and
therefore such adaptations and modifications are intended to be
comprehended within the meaning and range of equivalents of the disclosed
embodiments. It is to be understood that the phraseology or terminology
herein is for the purpose of description and not of limitation.
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